Lapatinib is a member of the 4-anilinoquinazoline class of kinase inhibitors. It is marketed in the USA as TYKERB® (Lapatinib) and is indicated in combination with: Capecitabine for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress HER2 and who have received prior therapy including an anthracycline, a taxane, and Trastuzumab and Letrozole for the treatment of postmenopausal women with hormone receptor positive metastatic breast cancer that overexpresses the HER2 receptor for whom hormonal therapy is indicated. Lapatinib inhibits ErbB-driven tumor cell growth in vitro and in various animal models. Lapatinib is present as the monohydrate of the ditosylate salt, with the chemical name N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-4-quinazolinaminebis(4-methylbenzenesulfonate)monohydrate.
U.S. Pat. No. 6,713,485 relates to substituted heteroaromatic compounds, methods for their preparation, pharmaceutical compositions containing them and their use in medicine. Specifically, the invention relates to quinazoline derivatives useful in treating disorders mediated by protein tyrosine kinase activity, in particular erbB-2 and/or EGFR activity
WO 2002/02552 discloses ditosylate salts of 4-quinazolineamines as well as methods of using the same in the treatment of disorders characterized by aberrant erbB family PTK activity.
WO 2010/017387 provides Lapatinib intermediates and improved processes for preparing Lapatinib intermediates. The invention also provides processes for preparing Lapatinib and Lapatinib ditosylate.
WO 2010/061400 relates to an improved and novel process for the preparation of high purity crystalline base of Lapatinib and its pharmaceutically acceptable salts. The invention further relates to intermediates according to formula (8) and formula (9) used in this process.